PEG

VHL-4

Nutlin-3a (Rebemadlin) is the active enantiomer of Nutlin-3 and serves as a potent inhibitor of murine double minute 2 (MDM2) with an IC50 of 90 nM. It disrupts the MDM2-p53 interaction, leading to stabilization of the p53 protein and subsequent induction of cell autophagy and apoptosis. Nutlin-3a is valuable for investigating TP53 wild-type ovarian carcinomas due to its structural specificity in targeting these interactions.

PT-179 is a Thalidomide derivative designed to specifically target cereblon without causing unintended degradation of other proteins. It binds to cereblon and forms a ternary complex with target proteins that are fused to a zinc finger (ZF) degron, facilitating their degradation. For instance, PT-179 interacts with cereblon and forms a complex with SD40, enabling efficient degradation of proteins tagged with SD40 or SD36. This makes PT-179 useful for developing targeted protein degradation systems.

AT-406 is a potent, orally bioavailable Smac mimetic that specifically targets inhibitor of apoptosis proteins (IAPs). It interacts with XIAP, cIAP1, and cIAP2, demonstrating high affinity for these proteins. This compound's structural design allows it to effectively bind and modulate the activity of these IAPs.

GDC-0152 is a highly effective inhibitor of inhibitor of apoptosis proteins (IAPs). It specifically targets the BIR3 domains of XIAP, cIAP1, and cIAP2, as well as the BIR domain of ML-IAP, demonstrating strong binding affinity across these proteins. Its structural design enables precise interaction with these domains, highlighting its role in modulating IAP activity.

3-(5-Bromo-3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidine-2,6-dione

VHL Ligand 14 is a ligand that interacts with the VHL E3 ligase, facilitating the development of PROTACs for targeting estrogen receptor α (ERα). Its structural properties enable effective binding and integration into degrader systems.

VL285 is a highly effective ligand for the VHL E3 ligase, featuring strong binding affinity. Its structural characteristics make it a valuable tool for applications involving VHL-mediated protein degradation.

TD-106 is a cereblon (CRBN) modulator that facilitates targeted protein degradation. It enables the use of BRD4 PROTACs to specifically promote the degradation of the BRD4 protein.